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dc.contributor.authorNirthanan, Selvanayagamen_US
dc.contributor.authorR. Ziebell, Michaelen_US
dc.contributor.authorC. Chiara, Daviden_US
dc.contributor.authorHong, Filberten_US
dc.contributor.authorB. Cohen, Jonathanen_US
dc.date.accessioned2017-05-03T15:29:01Z
dc.date.available2017-05-03T15:29:01Z
dc.date.issued2005en_US
dc.date.modified2009-09-28T06:52:27Z
dc.identifier.issn00062960en_US
dc.identifier.doi10.1021/bi051209yen_AU
dc.identifier.urihttp://hdl.handle.net/10072/25851
dc.description.abstractThe interactions of a photoreactive analogue of benzoylcholine, 4-azido-2,3,5,6-tetrafluorobenzoylcholine (APFBzcholine), with nicotinic acetylcholine receptors (nAChRs) were studied using electrophysiology and photolabeling. APFBzcholine acted as a low-efficacy partial agonist, eliciting maximal responses that were 0.3 and 0.1% of that of acetylcholine for embryonic mouse and Torpedo nAChRs expressed in Xenopus oocytes, respectively. Equilibrium binding studies of [3H]APFBzcholine with nAChR-rich membranes from Torpedo electric organ revealed equal affinities (Keq = 12 卩 for the two agonist binding sites. Upon UV irradiation at 254 nm, [3H]APFBzcholine was photoincorporated into the nAChR a, ?, and d subunits in an agonist-inhibitable manner. Photolabeled amino acids in the agonist binding sites were identified by Edman degradation of isolated, labeled subunit fragments. [3H]APFBzcholine photolabeled ?Leu-109/dLeu-111, ?Tyr-111, and ?Tyr-117 in binding site segment E as well as aTyr-198 in a subunit binding site segment C. The observed pattern of photolabeling is examined in relation to the predicted orientation of the azide when APFBzcholine is docked in the agonist binding site of a homology model of the nAChR extracellular domain based upon the structure of the snail acetylcholine binding protein.en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_AU
dc.languageEnglishen_US
dc.language.isoen_AU
dc.publisherAmerican Chemical Societyen_US
dc.publisher.placeWashington, DCen_US
dc.relation.ispartofstudentpublicationNen_AU
dc.relation.ispartofpagefrom13447en_US
dc.relation.ispartofpageto13456en_US
dc.relation.ispartofissue41en_US
dc.relation.ispartofjournalBiochemistryen_US
dc.relation.ispartofvolume44en_US
dc.rights.retentionYen_AU
dc.subject.fieldofresearchReceptors and Membrane Biologyen_US
dc.subject.fieldofresearchBasic Pharmacologyen_US
dc.subject.fieldofresearchcode060110en_US
dc.subject.fieldofresearchcode111501en_US
dc.titlePhotolabeling the Torpedo Nicotinic Acetylcholine Receptor with 4-Azido-2,3,5,6-tetrafluorobenzoylcholine, a Partial Agonisten_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.date.issued2005
gro.hasfulltextNo Full Text


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